Abstract
Positron emission tomography (PET) neuroimaging of ion channel linked receptors is a developing area of preclinical and clinical research. The present review focuses on recent advances with radiochemistry, preclinical and clinical PET imaging studies of three receptors that are actively pursued in neuropsychiatric drug discovery: namely the γ-aminobutyric acid-benzodiazapine (GABA) receptor, nicotinic acetylcholine receptor (nAChR), and N-methyl-D-aspartate (NMDA) receptor. Recent efforts to develop new PET radioligands for these targets with improved brain uptake, selectivity, stability and pharmacokinetics are highlighted.
Keywords: Positron Emission Tomography, Ion Channel, γ-Aminobutyric Acid-Benzodiazapine Receptor, Nicotinic Acetylcholine Receptor, N-Methyl-D-Aspartate Receptor.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors
Volume: 16 Issue: 16
Author(s): Alina Kassenbrock, Neil Vasdev and Steven H. Liang
Affiliation:
Keywords: Positron Emission Tomography, Ion Channel, γ-Aminobutyric Acid-Benzodiazapine Receptor, Nicotinic Acetylcholine Receptor, N-Methyl-D-Aspartate Receptor.
Abstract: Positron emission tomography (PET) neuroimaging of ion channel linked receptors is a developing area of preclinical and clinical research. The present review focuses on recent advances with radiochemistry, preclinical and clinical PET imaging studies of three receptors that are actively pursued in neuropsychiatric drug discovery: namely the γ-aminobutyric acid-benzodiazapine (GABA) receptor, nicotinic acetylcholine receptor (nAChR), and N-methyl-D-aspartate (NMDA) receptor. Recent efforts to develop new PET radioligands for these targets with improved brain uptake, selectivity, stability and pharmacokinetics are highlighted.
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Cite this article as:
Kassenbrock Alina, Vasdev Neil and H. Liang Steven, Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors, Current Topics in Medicinal Chemistry 2016; 16 (16) . https://dx.doi.org/10.2174/1568026616666160315142457
DOI https://dx.doi.org/10.2174/1568026616666160315142457 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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